Vaginal effects of ospemifene in the ovariectomized rat preclinical model of menopause was written by Unkila, Mikko;Kari, Seppo;Yatkin, Emrah;Lammintausta, Risto. And the article was included in Journal of Steroid Biochemistry and Molecular Biology in 2013.Computed Properties of C24H23ClO2 This article mentions the following:
Ospemifene is a unique tissue-selective estrogen agonist/antagonist (also known as a selective estrogen receptor modulator [SERM]) with demonstrated efficacy in Phase 3 studies of postmenopausal women with vulvar and vaginal atrophy (VVA). This report describes preclin. studies on the effects of ospemifene in the ovariectomized (OVX) rat model of menopause. Ospemifene (10 mg/kg/day) and the SERM comparator, raloxifene (10 mg/kg/day) were administered for 2 wk and both increased vaginal weight; ospemifene was more effective than raloxifene. In addition, ospemifene had a greater effect on increasing vaginal epithelial height compared with raloxifene. The effect on uterine weight was less pronounced for both ospemifene and raloxifene. The ED50 of ospemifene on vaginal epithelial height was 0.39 mg/kg/day and the magnitude was nearly the same as was seen with the pos. control, 17α-ethinyl estradiol (EE2). In a histol. anal. of ospemifene-treated rat vaginas, basal cells were overlaid by 2 to 3 cell layers of thickened goblet-like mucified cells apically; however, the cornification observed with EE2 was absent. Estrogenic activity of ospemifene was confirmed by upregulation of progesterone receptors in vaginal epithelium and stroma. Ospemifene showed similar affinity for estrogen receptor (ER)-α and ER-β, but an overall lower affinity than estradiol. Ospemifene antagonized estrogen response element (ERE)-mediated transactivation on MCF-7 cells, confirming its anti-estrogenic activity in breast cancer cells. The dose response for ospemifene in the rat is consistent with that observed in clin. studies of ospemifene 30 and 60 mg, showing that the OVX rat is a highly predictive model of SERM activity in postmenopausal VVA. In the experiment, the researchers used many compounds, for example, (Z)-2-(4-(4-Chloro-1,2-diphenylbut-1-en-1-yl)phenoxy)ethan-1-ol (cas: 128607-22-7Computed Properties of C24H23ClO2).
(Z)-2-(4-(4-Chloro-1,2-diphenylbut-1-en-1-yl)phenoxy)ethan-1-ol (cas: 128607-22-7) belongs to alcohols. Alkyl halides are often synthesized from alcohols, in effect substituting a halogen atom for the hydroxyl group. A multistep synthesis may use Grignard-like reactions to form an alcohol with the desired carbon structure, followed by reactions to convert the hydroxyl group of the alcohol to the desired functionality.Computed Properties of C24H23ClO2
Referemce:
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Alcohols – Chemistry LibreTexts